Advances in environmental engineering and green technologies book series,
Journal Year:
2024,
Volume and Issue:
unknown, P. 493 - 524
Published: Sept. 27, 2024
In
this
study
the
expression
of
drought-resistance
marker
genes
ZmNHL1,
ZmVPP1,
ZmNAC111:
antiradical
activity,
relative
water
content
and
biochemical
chromatographic
profiling
phenolic
compound
complex
in
leaves
maize
plants
treated
by
biopreparations
under
drought
stress,
was
investigated.
Drought
stress
significantly
affected
stress-responsive
action
(in
4-7
folds).
The
variant
with
«Organic-Balance®»
0.5
l/ha
+
«Azotohelp®»
0.3
«Liposam®»
0.25
were
characterized
high
total
compounds,
highest
activity
(88.2%),
most
active
glycosylation
processes
flavonoids
(up
to
13%),
(97.3%)
compared
control.
PCA
PLS-DA
showed
that
alterations
secondary
metabolites,
induced
biopreparations,
serve
as
an
initial
mechanism
for
activation
plant's
antioxidant
system,
leading
a
more
robust
defence
system
post-stress
signals.
Chemical Biology & Drug Design,
Journal Year:
2025,
Volume and Issue:
105(1)
Published: Jan. 1, 2025
ABSTRACT
Oxadiazole
compounds
are
of
great
interest
because
they
have
a
range
biological
activities
ranging
from
antioxidants
to
anticancer
agents.
Against
this
background,
we
wanted
demonstrate
the
antioxidant,
enzyme
inhibitory,
and
effects
5(4‐hydroxyphenyl)‐2‐(N‐phenylamino)‐1,3,4‐oxadiazole
(Hppo).
Antioxidant
abilities
were
measured
through
free
radical
scavenging
reducing
power
tests.
Enzyme
inhibitory
studied
by
cholinesterases,
tyrosinase,
amylase,
glucosidase.
The
effect
was
tested
on
pancreatic
cancer
cell
lines
(PANC‐1,
CRL‐169)
HEK293
lines.
compound
showed
significant
antioxidant
activity
(particularly
in
CUPRAC
(cupric
acid‐reducing
capacity)
assay)
properties
glucosidase
inhibition).
In
test,
strong
with
apoptotic
signaling
pathways.
These
results
confirmed
molecular
modeling
bioinformatics
tools.
Thus,
our
findings
can
provide
novel
versatile
for
development
multidirectional
drugs
pharmaceutical
industry.
Journal of Chemistry,
Journal Year:
2025,
Volume and Issue:
2025(1)
Published: Jan. 1, 2025
Antibiotic
resistance
represents
a
significant
public
health
challenge
in
the
current
century.
The
β‐lactam
antibiotics,
together
with
carbapenems,
are
inactivated
by
zinc‐dependent
bacterial
enzymes
called
metallo‐β‐lactamases
(MBLs).
Presently
there
no
clinically
permitted
MBL
inhibitors,
and
to
produce
such
drugs,
it
is
indispensable
comprehend
their
inhibitory
action.
We
investigated
an
efficient
synthesis
of
pyridine‐embedded
1,3,4‐oxadiazole
hybrids
(3a-c)
antimicrobial
activity
against
different
microbial
strains.
compounds
were
characterized
spectral
techniques
(viz.,
IR,
NMR,
mass).
vitro
antibacterial
antifungal
was
also
performed;
displayed
excellent
activity.
silico
docking
studies
evaluated
proteins
New
Delhi
Metallo-Beta-lactamase-1
(NDM‐1)
Mycobacterium
tuberculosis
enoyl
reductase
(INHA).
All
demonstrated
binding
affinity
for
docked
proteins.
Additionally,
molecular
dynamics
disclosed
(4a-c)
.
Chemical Biology & Drug Design,
Journal Year:
2024,
Volume and Issue:
103(6)
Published: June 1, 2024
Abstract
The
five‐membered
1,3,4‐oxadiazole
heterocyclic
ring
has
received
considerable
attention
because
of
its
unique
bio‐isosteric
properties
and
an
unusually
wide
spectrum
biological
activities.
After
a
century
since
was
discovered,
uncommon
potential
attracted
medicinal
chemist's
attention,
leading
to
the
discovery
few
presently
accessible
drugs
containing
units,
large
number
patents
have
been
granted
on
research
related
1,3,4‐oxadiazole.
It
is
worth
noting
that
interest
in
1,3,4‐oxadiazoles'
applications
doubled
last
years.
Herein,
this
review
presents
comprehensive
overview
recent
achievements
synthesis
1,3,4‐oxadiazole‐based
compounds
highlights
major
advances
their
10
years,
as
well
brief
remarks
prospects
for
further
development.
We
hope
researchers
across
scientific
streams
will
benefit
from
presented
articles
designing
work
1,3,4‐oxadiazoles.
Arabian Journal of Chemistry,
Journal Year:
2024,
Volume and Issue:
17(6), P. 105767 - 105767
Published: March 30, 2024
The
synthesis
and
biological
assessment
of
2,5-disubstituted-1,3,4-oxadiazole
derivatives
from
benzo
hydrazide
amino
acids
as
novel
potential
antioxidant
antibacterial
agents
have
been
reported.
structures
the
new
compounds
were
characterized
by
physicochemical
properties
spectral
methods.
synthesized
screened
for
their
in
vitro
activity
against
three
Gram-positive
bacterial
strains,
namely
Staphylococcus
aureus
ATCC
25923,
Bacillus
cereus
14579,
Listeria
innocua
33090,
two
Gram-negative
Pseudomonas
aeruginosa
27853,
Escherichia
coli
25922,
antifungal
Candida
albicans
10231
comparison
with
Amoxicillin,
Tetracycline,
Gentamicin
Oxacillin
standards.
Most
excellent
efficacy,
some
them,
such
5i,
5g,
5d,
5c,
5j
can
inhibit
better
or
very
close
to
that
Gentamicin,
used
Compounds
5b
5i
provided
good
results
L.
inhibition
values
IZ
=
14
mm
22
mm,
respectively,
while
rest
antibiotics
unable
it.
5g
showed
C.
between
31
34
mm.
These
than
all
standards
used.
MIC
value
(25
µg/ml)
5(c-e),
5(i-j)
B.
represent
best
tested
compounds.
All
target
also
radical
scavenging
activities
DPPH,
FRAP,
TAC
assays
found
be
agents.
According
results,
it
was
observed
most
a
concentration
250
µg/ml
an
agent
(76
%
<
RSA
95.5
%)
which
gave
percentage
ascorbic
acid
BHT.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(16), P. 6086 - 6086
Published: Aug. 16, 2023
We
report
herein
the
synthesis,
docking
studies
and
biological
evaluation
of
a
series
new
4-chloro-2-((5-aryl-1,3,4-oxadiazol-2-yl)amino)phenol
analogues
(6a-h).
The
compounds
were
designed
based
on
oxadiazole-linked
aryl
core
tubulin
inhibitors
IMC-038525
IMC-094332,
prepared
in
five
steps
further
characterized
via
spectral
analyses.
anticancer
activity
was
assessed
against
several
cancer
cell
lines
belonging
to
nine
different
panels
as
per
National
Cancer
Institute
(NCI
US)
protocol.
4-Chloro-2-((5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazol-2-yl)amino)phenol
(6h)
demonstrated
significant
SNB-19
(PGI
=
65.12),
NCI-H460
55.61),
SNB-75
54.68)
at
10
µM.
subjected
molecular
active
site
tubulin-combretastatin
A4
complex
(PDB
ID:
5LYJ);
they
displayed
efficient
binding
ligand
4h
(with
score
-8.030
kcal/mol)
lay
within
hydrophobic
cavity
surrounded
by
important
residues
Leu252,
Ala250,
Leu248,
Leu242,
Cys241,
Val238,
Ile318,
Ala317,
Ala316.
Furthermore,
antibacterial
some
found
be
promising.
4-Chloro-2-((5-(4-nitrophenyl)-1,3,4-oxadiazol-2-yl)amino)phenol
(6c)
most
promising
both
Gram-negative
well
Gram-positive
bacteria
with
MICs
8
µg/mL
zone
inhibition
ranging
from
17.0
±
0.40
0.15
mm
200
µg/mL;
however,
standard
drug
ciprofloxacin
exhibited
MIC
values
4
µg/mL.